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. 2021 May 22;26(11):3100. doi: 10.3390/molecules26113100

Scheme 23.

Scheme 23

Solid-phase CuAAC conjugation of oligonucleotides. Reagents and conditions: (a) solid-phase synthesis at 1 µmol scale, tetraazide (20 eq.), CuI·P(EtO)3 (2 eq.), 2 h, r.t. (b) solid-phase synthesis at 1 µmol scale, GalNAc-alkyne (10 eq.), CuI·P(EtO)3 (2 eq.), 2 h, r.t. (76.5% overall yield). (c) 1,2-ethylenediamine 2 h. (d) solid-phase synthesis at 1 µmol scale, tris-GalNAc-alkyne, (10 eq.), CuI·P(EtO)3, (2 eq.)2 h, r.t.